Patent SG-11201808678Q-A (SG)
Title: Macrocyclic inhibitors of the pd-1/pd-l1 and cd80/pd-l1 protein/protein interactions
Inventor: MILLER MICHAEL MATTHEW
IPC: C07K7/64
Filed: 2017-04-03
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 11M11111011101 11111111110101111101110101111111110011111110111111111110111111 International Bureau 0.. .... .. (10) International Publication Number ..... ...,/ (43) International Publication Date WO 2017/176608 Al 12 October 2017(12.10.2017) WIPO I PCT (51) International Patent Classification: ers Squibb Company, 5 Research Parkway, Wallingford, CO7K 7/54 (2006.01) A61P 31/00 (2006.01) Connecticut 06492 (US). LANGLEY, David R.; c/o Bris- CO7K 7/64 (2006.01) A61K 38/12 (2006.01) tol-Myers Squibb Company, 5 Research Parkway, Walling- A61P 35/00 (2006.01) ford, Connecticut 06492 (US). SCOLA, Paul Michael; c/o Bristol-Myers Squibb Company, 5 Research Parkway, (21) International Application Number: Wallingford, Connecticut 06492 (US). PCT/US2017/025677 (74) Agents: MINGO, Pamela A. et al.; Bristol-Myers Squibb (22) International Filing Date: Company, Route 206 and Province Line Road, Princeton, 3 April 2017 (03.04.2017) New Jersey 08543 (US). (25) Filing Language: English (81) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (30) Priority Data: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, 62/318,417 5 April 2016 (05.04.2016) US DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 15/475,227 31 March 2017 (31.03.2017) US HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (71) Applicant: BRISTOL-MYERS SQUIBB COMPANY KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, [US/US]; Route 206 and Province Line Road, Princeton, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, New Jersey 08543 (US). NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, (72) Inventors: MILLER, Michael Matthew; c/o Bristol-My- TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ers Squibb Company, Route 206 and Province Line Road, ZA, ZM, ZW. Princeton, New Jersey 08543 (US). ALLEN, Martin Patrick; c/o Bristol-Myers Squibb Company, Route 206 (84) Designated States (unless otherwise indicated, for every and Province Line Road, Princeton, New Jersey 08543 kind of regional protection available): ARIPO (BW, GH, (US). LI, Ling; c/o Bristol-Myers Squibb Company, Route GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, 206 and Province Line Road, Princeton, New Jersey 08543 TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (US). BOWSHER, Michael S.; c/o Bristol-Myers Squibb TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, Company, 5 Research Parkway, Wallingford, Connecticut DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, 06492 (US). GILLIS, Eric P.; c/o Bristol-Myers Squibb LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, Company, 5 Research Parkway, Wallingford, Connecticut SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, 06492 (US). MULL, Eric; c/o Bristol-Myers Squibb Com- GW, KM, ML, MR, NE, SN, TD, TG). pany, 5 Research Parkway, Wallingford, Connecticut Declarations under Rule 4.17: 06492 (US). ZHAO, Qian; 93 Hintz Drive, Wallingford, — as to applicant's entitlement to apply for and be granted a Connecticut 06492 (US). SUN, Li-Qiang; c/o Bristol-My- patent (Rule 4.1700) [Continued on next page] Title: MACROCYCLIC INHIBITORS OF THE PD-1/PD-L1 AND CD80/PD-L1 PROTEIN/PROTEIN INTERACTIONS = (54) R . Rt 0 R RI NN O R 5 Cr). Il R . a R1B(~ R z R14 R. . 4 „ GC © Rz z R . ,19 R. 15 NI. IN R . Il IN 1-1 (57) : The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L 1/CD80 0 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases. ” wherein: A is selected from a bond. O WO 2017/176608 Al MIDEDIMOMONIIMOIDEOMOIHHIMOOMODEVOIMIE • — as to the applicant's entitlement to claim the priority the earlier application (Rule 4.17(iii)) of '\"\"'\"\"' — with international search report (Art. 21(3)) — of inventorship (Rule 4.17(iv)) — with sequence listing part of description (Rule 5.2(a))